Prostate cancer is the second leading cause of new cancer cases in men worldwide and the six leading cause of cancer death in men. In the US, over two (2) million men currently suffer with prostate cancer and it is estimated that there were approximately 30,000 deaths due to the disease in 2008.
Diethylstilbestrol (DES) is a synthetic nonsteroidal estrogen (female sex hormone). It has been used in the treatment of both Androgen dependent and androgen-independent prostatic carcinoma. DES was the first effective drug for treatment of metastatic prostate cancer in 1941. It was first synthesized in London by Dodds in 1938. DES is inexpensive to manufacture however its biological properties are similar to those of naturally occurring expensive estrogens.
Oral diethylstilbestrol is an effective dosage form for the treatment of prostate cancer. It induces castrate serum testosterone levels. Studies have demonstrated that DES may improve the survival of patients with advanced prostate cancer compared with orchiectomy and luteinizing hormone-releasing hormone (LHRH). This is due to its positive effects on the bone by reducing osteoporosis and retarding the development of bond metastases. Oral DES therapy for prostate cancer is associated with excess cardiovascular side effects (heart attack, stroke and thrombosis). The cardiovascular side effects of DES are thought to be associated with DES metabolism in the liver. When estrogens are given orally, they are subject to intestinal and hepatic first-pass effect leading to high hormone concentrations in the liver promoting the synthesis of clotting proteins like fibrinogen.
Diethylstiltrol (DES) is effective in the treatment of both androgen dependent (ADPCa) and androgen-independent carcinoma (AIPCa). Oral DES therapy for prostate cancer is associated with excess cardiovascular side effects (heart attack, stroke and thrombosis). The cardiovascular side effects of DES are thought to be associated with DES metabolism in the liver. When estrogens are given orally, they are subject to intestinal and hepatic first-pass effect leading to high hormone concentrations in the liver promoting the synthesis of clotting proteins like fibrinogen.
US patent publication 2010/0016445 to Beer discloses methods for treating prostate cancer comprising transdermally administering a therapeutically effective amount of diethylstilbesterol (DES), or a pharmaceutically acceptable salt or complex thereof, to a subject. US patent publication 2003/0147936 discloses methods and products for the primary hormonal treatment of early stage, low and intermediate risk prostate cancers by prostatic implants of androgen suppressive drugs formulated as fused with a lipoid carrier or encapsulated in microcapsules or in Silastic capsules is provided. Such prostatic implants renders a constant slow-release of their contents to the prostate for extended periods by biodegradation and diffusion. These methods are designed to deliver long term low levels of DES. The present dosage form and method of treatment delivers high therapeutic levels DES quickly while avoiding the detrimental side effects.
Diethylstiltrol (DES) is effective in the treatment of both androgen dependent (ADPCa) and androgen-independent carcinoma (AIPCa).